A BRIEF REVIEW OF THE ANTICANCER ACTIVITY OF alpha-AMINOPHOSPHONIC ACID DERIVATIVES AND A REPORT ON THE IN VITRO ACTIVITY OF SOME DIALKYL alpha-aryl- (OR HETEROARYL)-alpha-(DIPHENYLMETHYLAMINO)METHANEPHOSPHONATES

Reports on the anticancer activity of representative alpha-aminophosphonic acid derivatives are briefly reviewed, with comments where possible on modes of action. Preliminary in vitro screening results are also presented for selected dialkyl alpha-aryl (or heteroaryl)-alpha-(diphenylmethylamino)methanephosphonates against the National Cancer Institute (NCI) 60-cell line panel of human tumor cells, which showed average response parameters for active compounds of GI(50) between 4.81 x 10(-6) and 2.40 x 10(-5) M, TGI between 1.88 and 6.28 x 10(-5) M, and LC50 between 5.71 and 9.37 x 10(-5) M. The highest activity was shown by the alpha-phenyl compound for which GI(50) 10(-7) M was recorded against leukemia cell line MOLT-4.